Ixazomib Citrate is a pharmaceutical active pharmaceutical ingredient belonging to the proteasome inhibitor class. It is the citrate salt of ixazomib and is used in oncology, particularly in pharmaceutical formulations for the treatment of multiple myeloma.
Ixazomib is an orally active, reversible proteasome inhibitor. It targets the 20S proteasome, an intracellular protein-degradation complex that regulates cellular protein homeostasis. Inhibition of the proteasome can cause accumulation of regulatory proteins within malignant plasma cells and contribute to inhibition of tumor-cell growth and survival.
Ixazomib Citrate has the molecular formula C14H19BCl2N2O4·C6H8O7 and a molecular weight of approximately 474.12 g/mol. It is identified by CAS Number 1072833-77-2.
Ixazomib Citrate is a boronic acid-containing pharmaceutical compound supplied in citrate salt form. The boronic acid functionality is important for its interaction with the catalytic site of the proteasome.
Ixazomib is a reversible inhibitor of the 20S proteasome. After administration, the active form of ixazomib binds to the proteasome and inhibits its chymotrypsin-like activity. This interferes with normal intracellular protein degradation and can result in accumulation of proteins that regulate cell-cycle progression and apoptosis, contributing to the death of susceptible myeloma cells.
Ixazomib Citrate is primarily used as an anticancer pharmaceutical ingredient for multiple myeloma. It is administered orally and is used in combination with other medicines, particularly lenalidomide and dexamethasone, in appropriate treatment settings.
Ixazomib Citrate API can be evaluated using validated analytical procedures for identity, assay, related substances, water content, residual solvents and elemental impurities. HPLC and other suitable chromatographic and spectroscopic techniques may be used for quality assessment.
Acceptance criteria for assay, impurities and other quality attributes should be based on the applicable approved drug-substance specification and Certificate of Analysis.
Ixazomib Citrate should be stored in a tightly closed pharmaceutical-grade container under controlled storage conditions. The material should be protected from excessive heat, moisture, direct light and contamination. Specific storage requirements should follow the applicable manufacturer's approved specification.
Ixazomib Citrate API may be supplied for qualified pharmaceutical manufacturing, formulation development, research and analytical applications. Product specifications, Certificate of Analysis, packaging details and regulatory documentation should be confirmed according to the intended application.
Ixazomib Citrate API is available for pharmaceutical development and manufacturing requirements subject to applicable quality and regulatory requirements. Customers can request product specifications, analytical documentation, Certificate of Analysis, packaging information and commercial details for their specific requirements.
| Parameter | Specification |
|---|---|
| Appearance | White to off-white crystalline powder |
| Identification | IR & HPLC compliant |
| Assay (HPLC) | 98.0% – 102.0% |
| Loss on Drying | NMT 1.0% |
| Residue on Ignition | NMT 0.5% |
| Individual Impurity | NMT 0.5% |
| Total Impurities | NMT 1.0% |
| Water Content | NMT 1.0% |